Assay Detail
Binding
CHEMBL4411170
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 0.5 nM DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosome as substrate and [3H]SAM as co-factor preincubated for 30 mins followed by substrate and cofactor addition and measured after 90 mins by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase, H3 lysine-79 specific (CHEMBL1795117) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
New Potent DOT1L Inhibitors for <i>in Vivo</i> Evaluation in Mouse.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.41 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448208 | — | — | 1 | 8.41 |
| CHEMBL4589340 | — | — | 1 | 7.80 |
| CHEMBL4587469 | — | — | 1 | 7.01 |
| CHEMBL4531049 | — | — | 1 | 6.57 |
| CHEMBL4456845 | — | — | 1 | 5.34 |
| CHEMBL4469355 | — | — | 1 | 5.07 |
| CHEMBL4563514 | — | — | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448208 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4589340 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4587469 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4531049 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4456845 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4469355 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4563514 | — | IC50 | = | 22800.0 | nM | 4.64 |